Diversity-oriented synthesis of a chemical library based on a pyrrolo[1,2-a]pyrazine core is described by using palladium-catalyzed direct C6 arylation of pyrrolo[1,2-a]pyrazines with various aryl bromides. The starting materials, pyrrolo[1,2-a]pyrazines, were easily synthesized by the base-mediated N-alkylation of pyrrole-2-carboxaldehyde with several 2-bromoacetophenones followed by dehydrative cyclization with incorporation of nitrogen by the action of ammonium acetate. Introduction of other functional groups on this chemical scaffold is also discussed herein.
|Number of pages||17|
|Publication status||Published - 2014 Oct 14|
Bibliographical noteFunding Information:
This research was supported in part by Nano Material Technology Development Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Education, Science and Technology . We also thank Yonsei University for partial financial support of this work through the Yonsei University Global Specialization Project of 2014.
© 2014 Elsevier Ltd. All rights reserved.
All Science Journal Classification (ASJC) codes
- Drug Discovery
- Organic Chemistry